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Wikipedia - Glimepiride

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Glimepiride
Systematic (IUPAC) name
3-ethyl-4-methyl-N-(4-[N-((1r,4r)-4-methylcyclohexylcarbamoyl)sulfamoyl]phenethyl)-2-oxo-2,5-dihydro-1H-pyrrole-1-carboxamide
Identifiers
CAS number 93479-97-1
ATC code A10BB12
PubChem CID 3476
DrugBank APRD00381
Chemical data
Formula C24H34N4O5S 
Mol. mass 490.617 g/mol
Pharmacokinetic data
Bioavailability 100%
Protein binding >99.5%
Half-life 5 Hours
Excretion Urine & Fecal
Therapeutic considerations
Pregnancy cat.  ?
Legal status
Routes Oral
 YesY(what is this?)  (verify)

Glimepiride is a medium-to-long acting sulfonylurea anti-diabetic drug. It is marketed as Amaryl by Sanofi-Aventis and Glista OD by Cadila Pharmaceuticals Ltd. Glimepiride is the first third-generation sulfonylurea, and is very potent.

It is sometimes classified as third-generation,[1] and sometimes classified as second-generation.[2]

Contents

[edit] Indications

Type 2 Diabetes Mellitus

[edit] Mode of Action

Glimepiride binds with Sulfonylurea receptor on the surface of Beta islet of pancreas. --> Blocks the K+ ion channels --> Cell undergoes depolarization --> Voltage dependent Ca++ ion channels open up --> Ca++ influx takes place --> Insulin sacs release insulin from beta islets of pancreas.

[edit] Adverse effects

Main article: Sulfonylurea

GI disturbance, rarely thrombocytopenia , leukopenia, hemolytic anemia, occasionally allergic reactions occur. In the initial weeks of treatment, the risk of hypoglycemia may be increased.

[edit] Contraindications

-Hypersensitivity to glimepiride or other sulfonylureas.

-Pregnancy

[edit] Interactions

With NSAIDs like Salicylates, Sulphonamides, Chloramphenicol, coumadin and probencid may potentiate the hypoglycemic action of glimepiride. Thiazides, other diuretic, phothiazides, thyroid products, oral contraceptives, phenytoin tend to produce hyperglycemia.

[edit] Pharmacokinetics

With glimepiride GI absorption is complete, with no interference of meals. Significant absorption of glimepiride was seen within 1 hour, and distributed throughout the body, bound to the plasma protein to an extent of 99.5% and it is metabolized by oxidative biotransformation and 60% is excreted in the urine, the remaining being excreted in the feces.

[edit] Pharmacodynamics

Main article: Sulfonylurea

Glimepiride lowers the blood glucose level by stimulating pancreatic beta cells to produce more insulin and by inducing increased activity of intracellular insulin receptors.

Not all secondary sufonylureas have the same risks of hypoglycemia. Glyburide has up to 20% to 30% incidence of hypoglycemia compared to 2% to 4% with glimepiride. Glyburide interfers with the normal homeostatic suppression of insulin secretion in reaction to hypoglycemia, whereas glimepiride does not have this property. Glyburide diminishes the glucagon secretion in reaction to hypoglycemia, whereas glimepiride does not suppress this counter-regulatory reaction.(Source: Goodman and Gilman's Pharmacological Basis of Therapeutics, 11 th edition, page 1636.)

It is considered a secretagogue.[3]

[edit] References

  1. ^ Hamaguchi T, Hirose T, Asakawa H, et al. (December 2004). "Efficacy of glimepiride in type 2 diabetic patients treated with glibenclamide". Diabetes Res. Clin. Pract. 66 Suppl 1: S129–32. doi:10.1016/j.diabres.2003.12.012. PMID 15563963. http://linkinghub.elsevier.com/retrieve/pii/S0168-8227(04)00148-2. 
  2. ^ Davis SN (2004). "The role of glimepiride in the effective management of Type 2 diabetes". J. Diabetes Complicat. 18 (6): 367–76. doi:10.1016/j.jdiacomp.2004.07.001. PMID 15531188. http://linkinghub.elsevier.com/retrieve/pii/S1056-8727(04)00078-9. 
  3. ^ Nissen SE, Nicholls SJ, Wolski K, et al. (April 2008). "Comparison of pioglitazone vs glimepiride on progression of coronary atherosclerosis in patients with type 2 diabetes: the PERISCOPE randomized controlled trial". JAMA 299 (13): 1561–73. doi:10.1001/jama.299.13.1561. PMID 18378631. http://jama.ama-assn.org/cgi/pmidlookup?view=long&pmid=18378631. 

[edit] External links

v â€¢ d â€¢ e
Oral anti-diabetic drugs and Insulin analogs (A10)
Insulin
Metformin# Â· Buformin‡ Â· Phenformin‡
Pioglitazone Â· Rivoglitazone† Â· Rosiglitazone Â· Troglitazone‡
Aleglitazar† Â· Muraglitazar§ Â· Tesaglitazar§
Meglitinides/"glinides"
Exenatide Â· Liraglutide Â· Taspoglutide† Â· Albiglutide†
Alogliptin† Â· Linagliptin† Â· Saxagliptin Â· Sitagliptin Â· Vildagliptin
Analogs/other insulins
fast acting (Insulin lispro Â· Insulin aspart Â· Insulin glulisine) Â· Short acting (Regular insulin) Â· long acting (Insulin glargine Â· Insulin detemir) Â· Inhalable insulin (Exubera)‡ Â· NPH insulin
Other
Amylin analog
SGLT2 inhibitors
Canagliflozin† Â· Dapagliflozin† Â· Remogliflozin† Â· Sergliflozin†
Other
Benfluorex Â· Tolrestat‡
#WHO-EM. ‡Withdrawn from market. CLINICAL TRIALS: †Phase III. §Never to phase III


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